Lyvelsa 10 mg

Indication:

Lyvelsa 10 mg is indicated for the treatment of –

• Chronic Kidney Disease (Stage 3 and 4 with albuminuria) associated with Type 2 Diabetes in adult patients.
• To reduce the risk of sustained eGFR decline, end-stage renal disease (ESRD), cardiovascular mortality, non-fatal myocardial infarction (heart attack), and hospitalization due to heart failure.

Dogase & Adminstration:

Adult Dose:The target maintenance dose of Finerenone is 20 mg once daily. The initiation dose is determined based on the patient’s baseline eGFR and serum potassium levels.

Dose Initiation Matrix:

• eGFR ≥ 60 mL/min/1.73 m²: Start with 20 mg once daily.
• eGFR ≥ 25 to 59 mL/min/1.73 m²: Start with 10 mg once daily.
• eGFR < 25 mL/min/1.73 m²: Avoid initiation due to limited clinical experience.

Up-titration (Dose Adjustment):

• Measure serum potassium and eGFR 4 weeks after initiation, restarting, or dose increment.
• If serum potassium is $le$ 4.8 mmol/L and eGFR is stable, the dose can be increased from 10 mg once daily to 20 mg once daily.

Dose Modification Based on Serum Potassium Monitoring:

• Potassium less 4.8 mmol/L: Maintain current dose or increase to 20 mg if on 10 mg.
• Potassium 4.9 – 5.4 mmol/L: Maintain current dose.
• Potassium > 5.5 mmol/L: Withhold Finerenone treatment. Monitor serum potassium closely. Restart at 10 mg once daily only when serum potassium levels drop to 5.0 mmol/L.

Child Dose:

• Pediatric Safety: Safety and efficacy have not been established in children and adolescents under 18 years of age. Therefore, Finerenone is not recommended for child use (absent in BNF for Children).

Method of Administration:

• Administer orally once daily at the same time every day, with or without food.
• Swallowing Difficulties: For patients unable to swallow whole tablets, Finerenone tablets may be crushed and mixed with water or soft foods (such as apple sauce) immediately before administration.
• Avoid consumption of grapefruit or grapefruit juice during treatment.

”রেজিস্ট্রার চিকিৎসকের পরামর্শ অনুযায়ী ঔষধ সেবন করুন”

Pharmacology:

Finerenone is a first-in-class, non-steroidal, selective mineralocorticoid receptor (MR) antagonist. Unlike traditional steroidal MRAs (such as spironolactone and eplerenone), finerenone exhibits a unique bulky non-steroidal structure that binds with high potency and selectivity to the MR, preventing aldosterone and cortisol-mediated receptor overactivation.

In patients with Chronic Kidney Disease (CKD) and Type 2 Diabetes, pathological MR overactivation triggers severe inflammatory cascades and progressive fibrotic pathways within the renal and cardiovascular tissues. Finerenone blocks these receptor-mediated pathways, resulting in:

1. Anti-inflammatory and Anti-fibrotic Effects: It downregulates the expression of pro-inflammatory cytokines and fibrotic markers, significantly halting structural kidney damage, glomerular sclerosis, and tubulointerstitial fibrosis.
2. Hemodynamic Stability: It reduces receptor-mediated sodium reabsorption without significantly lowering systemic blood pressure, providing potent organ protection.
3. Tissue Distribution: Finerenone distributes equally between heart and kidney tissues, offering balanced cardiorenal protection.

Side Effects:

Very Common / Common: Hyperkalemia (elevated blood potassium), hypotension (low blood pressure), hyponatremia (low blood sodium), pruritus (skin itching), and transient decrease in eGFR.

Drug Interaction:

• Strong CYP3A4 Inhibitors: Concomitant use with strong CYP3A4 inhibitors (e.g., itraconazole, ketoconazole, ritonavir, clarithromycin) is strictly contraindicated as it significantly increases finerenone plasma concentration.
• Moderate/Weak CYP3A4 Inhibitors: Medications like erythromycin, verapamil, amiodarone, or grapefruit juice may increase exposure; monitor serum potassium regularly.
• Potassium-Sparing Agents: Concomitant use of potassium supplements, trimethoprim, or potassium-sparing diuretics (e.g., spironolactone) increases the risk of severe hyperkalemia.

Pregnancy & Lactation:

• Pregnancy: Avoid unless the potential benefit outweighs the fetal risk. Animal studies have demonstrated reproductive toxicity.
• Lactation: Avoid breastfeeding during treatment. Animal studies show excretion of the drug into milk, causing adverse reactions in the exposed offspring.

Over Dosage:

• Symptoms: The most likely manifestation of an overdose is hyperkalemia.
• Management: Immediately discontinue Finerenone and initiate standard hyperkalemia treatment (e.g., insulin-glucose infusion, calcium gluconate, or potassium binders). Hemodialysis is not highly effective due to protein binding.

Therapeutic Class:

Potassium-sparing diuretics / Non-steroidal Mineralocorticoid Receptor Antagonists (MRAs).

Storage Conditions:

Store below at 30°C  temperature in a dry place. Away from light and out of reach of children. Do not use the medication after its expiration date.